JNJ 10181457 dihydrochloride
Cat. No. 4019
Chemical Name: 4-[3-[4-[Piperidinyl]but-1-ynyl]ben
Biological ActivityHistamine H3 receptor antagonist (pKi values are 8.15 and 8.93 for rat and human H3 receptors respectively). Increases extracellular norepinephrine and acetylcholine levels in rat frontal cortex but does not stimulate dopamine release. Brain penetrant.
Licensing InformationSold with the permission of Ortho-McNeil-Janssen Pharmaceuticals, Inc.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
Boggs et al (2009) JNJ-10181457, a selective non-imidazole histamine H3 receptor antagonist, normalizes acetylcholine neurotransmission and has efficacy in translational rat models of cognition. Neuropharmacology 56 1131. PMID: 19345233.
Esbenshade et al (2008) The histamine H3 receptor: an attractive target for the treatment of cognitive disorders. Br.J.Pharmacol. 154 1166. PMID: 18469850.
Bonaventure et al (2007) Histamine H3 receptor antagonists: from target identification to drug leads. Biochem.Pharmacol. 73 1084. PMID: 17129577.
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Citations are publications that use Tocris products. Selected citations for JNJ 10181457 dihydrochloride include:
Iida (2017) JNJ10181457, a histamine H3 receptor inverse agonist, regulates in vivo microglial functions and improves depression-like behaviours in mice. Biochem Biophys Res Commun 488 (3) 534. PMID: 28526411.
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